MS-444

生物活性靶点体外研究体内研究 MS-444 试剂级价格

MS-444

CAS号:150045-18-4
英文名:5,8-dihydroxy-3-methyl-4-(9H)-naphtho(2,3-c)furanone
中文名:MS-444
CBNumber:CB91339067
分子式:C13H10O4
分子量:230.22
MOL File:150045-18-4.mol

MS-444化学性质

沸点 :448.7±45.0 °C(Predicted)
密度 :1.452±0.06 g/cm3(Predicted)
酸度系数(pKa) :8.14±0.20(Predicted)
形态 :Solid
颜色 :Light yellow to brown

MS-444性质、用途与生产工艺

生物活性 MS-444 是平滑肌肌球蛋白轻链激酶 (MLCK) 的抑制剂，IC50 值为 10 μM。
靶点

IC50: 10 μM (myosin).
体外研究

MS-444 is a small molecule RNA-binding protein HuR (ELAVL1) inhibitor. Colorectal cancer (CRC) cells that display HuR overexpression are treated with MS-444 (1-100 μM) for 48 hr with IC ₅₀ s of 10.98±1.76 μM, 12.84±2.10 μM, 5.60±0.90 μM, 14.21±2.11 μM, and 10.98±1.24 μM for HCT116, HCA-7, RKO, HT-29, and SW480 cells, respectively. Growth inhibition is observed in all CRC lines with IC ₅₀ values ranging from 5.60 μM to 14.21 μM with observable effects seen at 10 μM MS-444. Contrasting effects are observed using non-transformed small intestinal (RIE-1 (IC ₅₀ =40.70±3.53 μM)) and colonic (YAMC (IC ₅₀ =28.16±3.23 μM)) epithelial cells. Both cell types display properties of normal intestinal epithelial cells and are proficient in 3′UTR AU-rich elements (ARE)-mRNA decay. Both non-transformed cell lines are ~3- to 4-fold less responsive to MS-444-mediated growth inhibition, with IC ₅₀ values of 40.70 μM and 28.16 μM ( P <0.05).
体内研究

To test the effects of MS-444 on CRC cell growth in vivo, mice bearing HCT116 cell xenografts receive IP injections of MS-444 (25 mg/kg bw) or vehicle every 48 hr. Over the experiment course, mice do not display any adverse effects and maintained similar weights. Anti-tumor effects of MS-444 are observed with approximately 1.7-fold reduction in tumor size. Mice treated with MS-444 show a marked 2- to 3-fold decrease in microvessel density (MVD), indicating the anti-angiogenic potential of MS-444.